Sesquiterpene Furan Compound CJ-01, a Novel Chitin Synthase 2 Inhibitor from Chloranthus japonicus S<small>IEB</small>.

Nam Hui Yim; Eui Il Hwang; Bong Sik Yun; Ki Duk Park; Jae Sun Moon; Sang Han Lee; Nack Do Sung; Sung Uk Kim

doi:10.1248/bpb.31.1041

Notes

Sesquiterpene Furan Compound CJ-01, a Novel Chitin Synthase 2 Inhibitor from Chloranthus japonicus SIEB.

Nam Hui Yim, Eui Il Hwang, Bong Sik Yun, Ki Duk Park, Jae Sun Moon, Sang Han Lee, Nack Do Sung, Sung Uk Kim

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Keywords: fungal cell wall, chitin synthase 2 inhibitor, Chloranthus japonicus, sesquiterpene furan compound CJ-01, antifungal activity

JOURNAL FREE ACCESS

2008 Volume 31 Issue 5 Pages 1041-1044

DOI https://doi.org/10.1248/bpb.31.1041

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Abstract

A novel sesquiterpene furan compound CJ-01 was isolated from the methanol extract of the whole plant of Chloranthus japonicus SIEB. by monitoring the inhibitory activity of chitin synthase 2 from Saccharomyces cerevisiae. Based on spectroscopic analysis, the structure of compound CJ-01 was determined as 3,4,8a-trimethyl-4a,7,8,8a-tetrahydro-4a-naphto[2,3-b]furan-9-one. The compound inhibited chitin synthase 2 of Saccharomyces cerevisiae in a dose-dependent manner with an IC₅₀ of 39.6 μg/ml, whereas it exhibited no inhibitory activities against chitin synthase 1 and 3 of S. cerevisiae up to 280 μg/ml. CJ-01 has 1.7-fold stronger inhibitory activity than polyoxin D (IC₅₀=70 μg/ml), a well-known chitin synthase inhibitor. These results indicate that the compound is a specific inhibitor of chitin synthase 2 from S. cerevisiae. In addition, CJ-01 showed antifungal activities against various human and phytopathogenic fungi. Therefore, the compound might be an interesting lead to develop effective antifungal agents.

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